Forsythiaside, as an aglycon part of forsythin, is also known as phillygenin, is a main active component of Forsythia suspensa of the genus Forsythia in, the family Oleaceae and has a structure as represented below. Modern pharmacological researches show that forsythiaside has antiviral, antioxidant, lowering blood lipid scavenging free radical, antibacterial, antitumor, anti-inflammatory effect and the like.

Forsythiaside has unstable molecules which is prone to oxidized and easy to change the configuration in an acidic environment. Researches simulating forsythin metabolism through rat enteric bacteria discover that forsythin is easily metabolized by intestinal flora into a new metabolite.
Researches on metabolism of phenolic structural drugs discover that drugs with the structural of phenolic hydroxylare easily metabolized by in-vivo sulfatases into phenol sulfate derivatives and have good activity. For example, daidzein sulfate derivatives, edaravone sulfate derivatives, genistein sulfate derivatives, resveratrol sulfate derivatives and the like. Therefore, we designed sulfate derivatives of phillygenin and carried out chemical synthesis and pharmacological studies.